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PE64598A1 - SUBSTITUTED INDAZOL DERIVATIVES AND RELATED COMPOUNDS - Google Patents

SUBSTITUTED INDAZOL DERIVATIVES AND RELATED COMPOUNDS

Info

Publication number
PE64598A1
PE64598A1 PE1997000330A PE00033097A PE64598A1 PE 64598 A1 PE64598 A1 PE 64598A1 PE 1997000330 A PE1997000330 A PE 1997000330A PE 00033097 A PE00033097 A PE 00033097A PE 64598 A1 PE64598 A1 PE 64598A1
Authority
PE
Peru
Prior art keywords
formula
compounds
preference
related compounds
double link
Prior art date
Application number
PE1997000330A
Other languages
Spanish (es)
Inventor
Anthony Marfat
Original Assignee
Pfizer
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Pfizer filed Critical Pfizer
Publication of PE64598A1 publication Critical patent/PE64598A1/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56Benzopyrazoles; Hydrogenated benzopyrazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/08Bronchodilators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/02Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • A61P33/02Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/08Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing alicyclic rings
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Transplantation (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Urology & Nephrology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

SE REFIEREN A COMPUESTOS DE FORMULA (I) Y A COMPUESTOS INTERMEDIOS DE FORMULA (XV) Y (XIX), EN DONDE: R ES H, ALQUILO C1-C6 O (CH2)n(CICLOALQUILO C3-C7), ENTRE OTROS, EN DONDE: n ES 0; 1 o 2; SIENDO DE PREFERENCIA R UN CICLOHEXILO O CICLOPENTILO; R1 ES DE PREFERENCIA ETILO; R2 ES DE PREFERENCIA (Ia), EN DONDE LAS LINEAS DISCONTINUAS SON UN ENLACE SENCILLO O DOBLE, CON LA CONDICION DE QUE SI R5 ESTA AUSENTE CUANDO LA LINEA DISCONTINUA EN LA FORMULA (Ia) ES UN DOBLE ENLACE; R3 ES H O CN, ENTRE OTROS; R4 ES CARBOXI, CH2OH O CH2CONH2, ENTRE OTROS; R5 ES R9, OR9 O CH2OR9, ENTRE OTROS; O R4 Y R5 SE UNEN PARA FORMAR =O o =R8; R8 ES =NCN O =NCR9R10(ALQUENILO C2-C6), ENTRE OTROS; R9 Y R10 SON H O ALQUILO C1-C4 OPCIONALMENTE SUSTITUIDO HASTA CON 3 FLUOR. ESTOS COMPUESTOS ACTUAN COMO INHIBIDORES SELECTIVOS DE LA FOSFODIESTERASA (PDE) TIPO IV Y DE LA PRODUCCION DEL FACTOR DE NECROSIS TUMORAL, SIENDO UTIL EN EL TRATAMIENTO DEL ASMA, DE LA ARTRITIS REUMATOIDEA, ENTRE OTROSTHEY REFER TO COMPOUNDS OF FORMULA (I) AND INTERMEDIATE COMPOUNDS OF FORMULA (XV) AND (XIX), WHERE: R ES H, ALQUILO C1-C6 O (CH2) n (CICLOALQUILO C3-C7), AMONG OTHERS, WHERE : n IS 0; 1 or 2; BEING OF PREFERENCE R A CYCLOHEXILO OR CICLOPENTILO; R1 IS PREFERRED ETHYL; R2 IS OF PREFERENCE (Ia), WHERE THE DISCONTINUOUS LINES ARE A SIMPLE OR DOUBLE LINK, WITH THE CONDITION THAT IF R5 IS ABSENT WHEN THE DISCONTINUOUS LINE IN THE FORMULA (Ia) IS A DOUBLE LINK; R3 IS H O CN, AMONG OTHERS; R4 IS CARBOXY, CH2OH OR CH2CONH2, AMONG OTHERS; R5 IS R9, OR9 OR CH2OR9, AMONG OTHERS; OR R4 AND R5 JOIN TO FORM = O or = R8; R8 ES = NCN O = NCR9R10 (C2-C6 ALKYNYLL), AMONG OTHERS; R9 AND R10 ARE H OR C1-C4 ALKYL OPTIONALLY REPLACED UP TO 3 FLUORESCENT. THESE COMPOUNDS ACT AS SELECTIVE INHIBITORS OF TYPE IV PHOSPHODIESTERASE (PDE) AND OF THE PRODUCTION OF THE TUMOR NECROSIS FACTOR, BEING USEFUL IN THE TREATMENT OF ASTHMA, RHEUMATOID ARTHRITIS, AMONG OTHERS

PE1997000330A 1996-05-03 1997-04-30 SUBSTITUTED INDAZOL DERIVATIVES AND RELATED COMPOUNDS PE64598A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US1686196P 1996-05-03 1996-05-03

Publications (1)

Publication Number Publication Date
PE64598A1 true PE64598A1 (en) 1998-10-26

Family

ID=21779401

Family Applications (1)

Application Number Title Priority Date Filing Date
PE1997000330A PE64598A1 (en) 1996-05-03 1997-04-30 SUBSTITUTED INDAZOL DERIVATIVES AND RELATED COMPOUNDS

Country Status (41)

Country Link
US (2) US6211222B1 (en)
EP (1) EP0912521B1 (en)
JP (1) JP3148254B2 (en)
KR (1) KR100339935B1 (en)
CN (2) CN1112359C (en)
AP (4) AP2001002304A0 (en)
AR (1) AR006906A1 (en)
AT (1) ATE292626T1 (en)
AU (1) AU725576B2 (en)
BG (1) BG64211B1 (en)
BR (1) BR9709051A (en)
CA (2) CA2252982C (en)
CO (1) CO4650038A1 (en)
CZ (1) CZ292825B6 (en)
DE (1) DE69732966T2 (en)
DZ (1) DZ2217A1 (en)
EA (1) EA002272B1 (en)
ES (1) ES2238079T3 (en)
GT (1) GT199700043A (en)
HN (1) HN1997000046A (en)
HR (1) HRP970227B1 (en)
HU (1) HUP9902459A3 (en)
ID (1) ID16856A (en)
IL (2) IL152083A0 (en)
IS (1) IS4871A (en)
MA (1) MA24158A1 (en)
MY (1) MY132499A (en)
NO (1) NO312959B1 (en)
NZ (1) NZ332240A (en)
OA (1) OA10904A (en)
PE (1) PE64598A1 (en)
PL (1) PL329836A1 (en)
SK (1) SK148298A3 (en)
TN (1) TNSN97070A1 (en)
TR (1) TR199802202T2 (en)
TW (1) TW449585B (en)
UA (1) UA65536C2 (en)
UY (1) UY24532A1 (en)
WO (1) WO1997042174A1 (en)
YU (1) YU16397A (en)
ZA (1) ZA973804B (en)

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US6005118A (en) * 1996-05-03 1999-12-21 Caron; Stephane Methods of preparing 4-cyano-4 (substituted indazole) cyclohexane-carboxylic acids useful as PDE4 inhibitors
AP2001002304A0 (en) * 1996-05-03 2001-12-31 Pfizer Substituted indazole derivatives and related compounds
EP2223920A3 (en) 1996-06-19 2011-09-28 Aventis Pharma Limited Substituted azabicyclic compounds
WO1998050367A1 (en) * 1997-05-08 1998-11-12 Pfizer Products Inc. Processes and intermediates for preparing substituted indazole derivatives
TR200001256T2 (en) * 1997-11-04 2000-11-21 Pfizer Products Inc. Therapeutically active compositions.
IL126745A (en) 1997-11-04 2003-09-17 Pfizer Prod Inc Methods of preparing 4-cyano-4- (substituted indazole) cyclohexanecarboxylic acids useful as pde4 inhibitors
ID23921A (en) * 1997-11-04 2000-05-25 Pfizer Prod Inc REPLACEMENT OF INDAZOLA BIOISOSTERE CATEGOL IN ACTIVE COMPOUNDS FOR THERAPY
IL132407A0 (en) * 1998-10-21 2001-03-19 Pfizer Prod Inc Method for treating congestive heart failure
JP2000198734A (en) * 1998-12-30 2000-07-18 Pfizer Inc Motility enhancers for the treatment of gastric motility impairment and related disorders
US6303782B1 (en) * 1999-04-20 2001-10-16 Pfizer Inc Process for preparing benzylnitriles
US6362213B1 (en) 1999-12-23 2002-03-26 Icos Corporation Cyclic AMP-specific phosphodiesterase inhibitors
AU770918B2 (en) * 1999-12-23 2004-03-11 Icos Corporation Cyclic AMP-specific phosphodiesterase inhibitors
US7211594B2 (en) * 2000-07-31 2007-05-01 Signal Pharmaceuticals, Llc Indazole compounds and compositions thereof as JNK inhibitors and for the treatment of diseases associated therewith
US6897231B2 (en) * 2000-07-31 2005-05-24 Signal Pharmaceuticals, Inc. Indazole derivatives as JNK inhibitors and compositions and methods related thereto
US6953774B2 (en) 2000-08-11 2005-10-11 Applied Research Systems Ars Holding N.V. Methods of inducing ovulation
IL162506A0 (en) 2001-12-14 2005-11-20 Applied Research Systems Ovulation induction
US20040034084A1 (en) * 2002-05-24 2004-02-19 Celgene Corporation Methods for using JNK inhibitors for treating or preventing disease-related wasting
US7196082B2 (en) * 2002-11-08 2007-03-27 Merck & Co. Inc. Ophthalmic compositions for treating ocular hypertension
US20050019366A1 (en) * 2002-12-31 2005-01-27 Zeldis Jerome B. Drug-coated stents and methods of use therefor
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US7601847B2 (en) 2004-10-26 2009-10-13 Wyeth Preparation and purification of 4-(indazol-3-yl)phenols
US20070004777A1 (en) * 2005-03-23 2007-01-04 Bhagwat Shripad S Methods for treating or preventing acute myelogenous leukemia
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WO2007047978A2 (en) 2005-10-21 2007-04-26 Braincells, Inc. Modulation of neurogenesis by pde inhibition
EP1942879A1 (en) 2005-10-31 2008-07-16 Braincells, Inc. Gaba receptor mediated modulation of neurogenesis
US20100216734A1 (en) 2006-03-08 2010-08-26 Braincells, Inc. Modulation of neurogenesis by nootropic agents
AU2007240355B2 (en) * 2006-04-21 2013-09-26 Centocor, Inc. CXCL13 antagonists and their use for the treatment of inflammatory diseases
JP2009536669A (en) 2006-05-09 2009-10-15 ブレインセルス,インコーポレイティド Neurogenesis by angiotensin regulation
US20100184806A1 (en) 2006-09-19 2010-07-22 Braincells, Inc. Modulation of neurogenesis by ppar agents
WO2010099217A1 (en) 2009-02-25 2010-09-02 Braincells, Inc. Modulation of neurogenesis using d-cycloserine combinations
WO2013106547A1 (en) 2012-01-10 2013-07-18 President And Fellows Of Harvard College Beta-cell replication promoting compounds and methods of their use
KR20200104291A (en) 2017-11-06 2020-09-03 랩트 테라퓨틱스, 인크. Anticancer drugs

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Also Published As

Publication number Publication date
IL152083A0 (en) 2003-05-29
CN1422849A (en) 2003-06-11
HN1997000046A (en) 1997-06-26
NZ332240A (en) 2000-07-28
CZ292825B6 (en) 2003-12-17
DE69732966D1 (en) 2005-05-12
HUP9902459A3 (en) 2001-10-29
PL329836A1 (en) 1999-04-12
CN1112359C (en) 2003-06-25
CA2252982A1 (en) 1997-11-13
EA002272B1 (en) 2002-02-28
US6127398A (en) 2000-10-03
ZA973804B (en) 1998-11-02
HRP970227A2 (en) 2000-12-31
AU725576B2 (en) 2000-10-12
ATE292626T1 (en) 2005-04-15
AP9700975A0 (en) 1997-07-31
JPH11508284A (en) 1999-07-21
YU16397A (en) 1999-12-27
CA2252982C (en) 2002-10-08
ES2238079T3 (en) 2005-08-16
EP0912521A1 (en) 1999-05-06
TR199802202T2 (en) 1999-02-22
UA65536C2 (en) 2004-04-15
ID16856A (en) 1997-11-13
OA10904A (en) 2001-10-11
CA2389918A1 (en) 1997-11-13
JP3148254B2 (en) 2001-03-19
AR006906A1 (en) 1999-09-29
US6211222B1 (en) 2001-04-03
DE69732966T2 (en) 2005-09-08
BG102946A (en) 1999-11-30
TW449585B (en) 2001-08-11
KR20000010751A (en) 2000-02-25
MA24158A1 (en) 1997-12-31
WO1997042174A1 (en) 1997-11-13
IL126547A0 (en) 1999-08-17
BG64211B1 (en) 2004-05-31
NO985095D0 (en) 1998-11-02
KR100339935B1 (en) 2002-07-18
CO4650038A1 (en) 1998-09-03
CZ349298A3 (en) 1999-09-15
IS4871A (en) 1998-10-16
NO985095L (en) 1998-12-29
TNSN97070A1 (en) 2005-03-15
AP2001002294A0 (en) 2001-12-31
UY24532A1 (en) 2000-09-29
BR9709051A (en) 1999-08-03
AP1146A (en) 2003-02-25
AU1937397A (en) 1997-11-26
IL126547A (en) 2003-03-12
HRP970227B1 (en) 2002-06-30
DZ2217A1 (en) 2002-12-03
AP0102304A0 (en) 1997-11-03
GT199700043A (en) 1998-10-02
HUP9902459A2 (en) 1999-11-29
AP1147A (en) 2003-02-25
NO312959B1 (en) 2002-07-22
EA199800882A1 (en) 1999-06-24
HK1019443A1 (en) 2000-02-11
MY132499A (en) 2007-10-31
EP0912521B1 (en) 2005-04-06
CN1217714A (en) 1999-05-26
SK148298A3 (en) 2000-02-14
AP2001002304A0 (en) 2001-12-31

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